Effect of urea-treatment on agonist binding affinity of the muscarinic acetylcholine receptor |
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Authors: | Kazuo Matsumoto Shuji Uchida Hiroshi Higuchi Atsushi Mizushima Hiroshi Yoshida |
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Affiliation: | Department of Pharmacology I, Osaka University School of Medicine, Nakanoshima, Kita-ku, Osaka 530, Japan |
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Abstract: | Urea-treatment of the microsome fraction of the heart of guinea-pigs caused selective reduction in the apparent affinity of an agonist (carbachol), but not an antagonist (atropine), to muscarinic acetylcholine receptors (mAChR), measured as inhibition of binding of 3H-quinuclidinyl benzilate (3H-QNB). This effect was similar to that of Gpp(NH)p. The effects of urea-treatment and Gpp(NH)p were not additive. On the other hand, treatment of the microsome fraction with 5,5′-dithiobis (2-nitrobenzoic acid) (DTNB) increased the apparent affinity of agonist, but not antagonist. The effect of DTNB predominated over those of urea-treatment and Gpp(NH)p, when these treatments were combined with DTNB. |
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